Pilot in vivo structure-activity relationship of dihydromethysticin in blocking 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone-induced O6-methylguanine and lung tumor in A/J mice

摘要

(+)-Dihydromethysticin was recently identified as a promising lung cancer chemopreventive agent while (+)-dihydrokavain was completely ineffective. A pilot in vivo structure-activity relationship (SAR) was explored, evaluating the efficacy of its analogs in blocking 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone-induced short-term O⁶-methylguanine and long-term adenoma formation in the lung tissues in A/J mice. Both results revealed cohesive SARs, demonstrating that the methylenedioxy functional group in DHM is essential while the lactone functional group tolerates modifications.